CAS 29094-61-9|Glipizide

Introduction：Basic information about CAS 29094-61-9|Glipizide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Glipizide BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles22
8. Synonyms

Common Name	Glipizide
CAS Number	29094-61-9	Molecular Weight	445.535
Density	1.4±0.1 g/cm3	Boiling Point	676.0±65.0 °C at 760 mmHg
Molecular Formula	C₂₁H₂₇N₅O₄S	Melting Point	208-209°C
MSDS	USA	Flash Point	362.6±34.3 °C

Names

Name	glipizide
Synonym	More Synonyms

Glipizide BiologicalActivity

Description	Glipizide(K 4024; CP 2872) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.Target: Potassium ChannelGlipizide is an oral rapid- and short-acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues [1, 2].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Metabolic Disease
References	[1]. Chowdary, K.P. and Y.S. Rao, Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech, 2003. 4(3): p. E39. [2]. Rao, N.G., et al., Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law, 2006. 46(3): p. 263-9.

Description

Glipizide(K 4024; CP 2872) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.Target: Potassium ChannelGlipizide is an oral rapid- and short-acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues [1, 2].

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Metabolic Disease

References

[1]. Chowdary, K.P. and Y.S. Rao, Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech, 2003. 4(3): p. E39.

[2]. Rao, N.G., et al., Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law, 2006. 46(3): p. 263-9.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	676.0±65.0 °C at 760 mmHg
Melting Point	208-209°C
Molecular Formula	C₂₁H₂₇N₅O₄S
Molecular Weight	445.535
Flash Point	362.6±34.3 °C
Exact Mass	445.178375
PSA	138.53000
LogP	3.37
Vapour Pressure	0.0±2.2 mmHg at 25°C
Index of Refraction	1.654
InChIKey	ZJJXGWJIGJFDTL-UHFFFAOYSA-N
SMILES	Cc1cnc(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc2)cn1
Storage condition	-20°C Freezer
Water Solubility	methanol: 1.9 mg/mL

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YS7640000

CHEMICAL NAME :: Urea, 1-cyclohexyl-3-((p-(2-(5-methylpyrazinecarboxamido)et hyl)phenyl)sulfonyl)-

CAS REGISTRY NUMBER :: 29094-61-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C21-H27-N5-O4-S

MOLECULAR WEIGHT :: 445.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 2400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

Safety Information

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi: Irritant;Xn: Harmful;
Risk Phrases	R21
Safety Phrases	S24/25
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	YS7640000
HS Code	2935009090

Customs

HS Code	2935009090
Summary	2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Articles22

Identification of CYP3A7 for glyburide metabolism in human fetal livers.

Biochem. Pharmacol. 92(4) , 690-700, (2014)

Glyburide is commonly prescribed for the treatment of gestational diabetes mellitus; however, fetal exposure to glyburide is not well understood and may have short- and long-term consequences for the ...

Maternal-fetal disposition of glyburide in pregnant mice is dependent on gestational age.

J. Pharmacol. Exp. Ther. 350(2) , 425-34, (2014)

Gestational diabetes mellitus is a major complication of human pregnancy. The oral clearance (CL) of glyburide, an oral antidiabetic drug, increases 2-fold in pregnant women during late gestation vers...

Quantitative determination of metformin, glyburide and its metabolites in plasma and urine of pregnant patients by LC-MS/MS.

Biomed. Chromatogr. 29(4) , 560-9, (2015)

This report describes the development and validation of an LC-MS/MS method for the quantitative determination of glyburide (GLB), its five metabolites (M1, M2a, M2b, M3 and M4) and metformin (MET) in ...

Synonyms

EINECS 249-427-6

N-[2-(4-{[(E)-(Cyclohexylimino)(hydroxy)methyl]sulfamoyl}phenyl)ethyl]-5-methyl-2-pyrazinecarboximidic acid

Glican

Ozidia

N-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phényl}éthyl)-5-méthylpyrazine-2-carboxamide

Glipid

N-(2-{4-[(Cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-5-methyl-2-pyrazinecarboxamide

k4024

N-(2-{4-[(Cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-5-methylpyrazin-2-carboxamid

N-(2-{4-[(cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-5-methylpyrazine-2-carboxamide

exylurea

2-Pyrazinecarboxamide, N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-5-methyl-

Pyrazinecarboxamide, N-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-5-methyl-

Glucotrol

Glipizide

MFCD00072159

N-[4-(3-Cyclohexylureidosulfonyl)phenethyl]-5-methyl-2-pyrazinecarboxamide

Mindiab

Digrin

Glibenese

Glidiab

1-Cyclohexyl-3-{4-[2-(5-methylpyrazine-2-carboxamido)ethyl]phenylsulfonyl}urea

tk1320

Aldiab

2-Pyrazinecarboximidic acid, N-[2-[4-[[[(E)-(cyclohexylimino)hydroxymethyl]amino]sulfonyl]phenyl]ethyl]-5-methyl-

Melizide

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